167402-12-2

Upstream product

• 4013-71-2 pyridine-2-carbonyl azide 
• 150726-49-1 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-2-isopropyl-5-(2-methoxy-phenoxy)-pyrimidin-4-yl]-benzenesulfonamide 
• 150727-05-2 4,6-Dichloro-2-isopropyl-5-(2-methoxy-phenoxy)-pyrimidine 

Relevant academic research and scientific papers

Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from Bosentan

Implementation of a pyridylcarbamoyl group and an isopropylpyridylsulfonamide substituent as key components in the scaffold of Bosentan resulted in the identification of the potent orally active endothelin receptor antagonist Ro 48-5695. It shows affinities for ET(A) and ET(B) receptors in the low nanomolar range and high functional antagonistic potency in vitro.

SULFONYLAMINOPYRIMIDINES

A compound of the formula STR1 wherein R 1 to R, R a, R. sup.b X, Y, Z, m and n have the significance given in the description, can be used as medicaments, especially for the treatment and prophylaxix of conditions which are associated with endothelin activities.